Rosuvastatin and Antacids: Impact on Pharmacokinetics and Clinical Implications
How does a combination antacid containing aluminium hydroxide and magnesium hydroxide affect rosuvastatin pharmacokinetics. What are the implications for simultaneous and separated administration of these medications. How can healthcare providers optimize rosuvastatin efficacy when co-administered with antacids.
Understanding Rosuvastatin: A Powerful HMG-CoA Reductase Inhibitor
Rosuvastatin is a potent member of the statin class of medications, specifically designed to treat dyslipidemia. As a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, it plays a crucial role in managing cholesterol levels and reducing cardiovascular risk. Given its widespread use, it’s essential to understand how rosuvastatin interacts with other commonly used medications, such as antacids.
Key Features of Rosuvastatin
- Potent HMG-CoA reductase inhibitor
- Used primarily for treating dyslipidemia
- Helps reduce LDL cholesterol and triglycerides
- Increases HDL cholesterol levels
- Contributes to overall cardiovascular risk reduction
Can rosuvastatin be affected by other medications? Indeed, like many drugs, rosuvastatin’s efficacy can be influenced by co-administered substances, including over-the-counter products like antacids.
The Interplay Between Rosuvastatin and Antacids: A Clinical Concern
The potential interaction between rosuvastatin and antacids has been a subject of clinical interest. Antacids, particularly those containing aluminium hydroxide and magnesium hydroxide (co-magaldrox), are commonly used to alleviate symptoms of acid reflux and indigestion. Understanding how these substances interact is crucial for optimizing treatment outcomes.
Components of the Studied Antacid Preparation
- Aluminium hydroxide: 220 mg/5 mL
- Magnesium hydroxide: 195 mg/5 mL
How might these antacid components affect rosuvastatin’s pharmacokinetics? This question formed the basis of a comprehensive clinical trial designed to elucidate the nature and extent of this interaction.
Clinical Trial Design: Assessing the Rosuvastatin-Antacid Interaction
To investigate the potential interaction between rosuvastatin and antacids, researchers conducted a randomized, open-label, three-way crossover trial. This study design allows for a thorough comparison of different administration scenarios while minimizing inter-individual variability.
Trial Parameters
- Participants: 14 healthy male volunteers
- Rosuvastatin dose: 40 mg (single dose)
- Antacid dose: 20 mL of suspension
- Washout period: ≥7 days between each administration
Administration Scenarios
- Rosuvastatin 40 mg alone
- Rosuvastatin 40 mg plus antacid taken simultaneously
- Rosuvastatin 40 mg followed by antacid 2 hours later
Why is the timing of antacid administration important? The study aimed to determine if the timing of antacid intake relative to rosuvastatin dosing could mitigate any potential interactions.
Pharmacokinetic Parameters: Measuring the Impact of Antacids
To quantify the effect of antacids on rosuvastatin pharmacokinetics, researchers focused on two primary parameters:
- AUC(0-t): Area under the rosuvastatin plasma concentration-time curve from time zero to the last quantifiable concentration
- C(max): Maximum observed rosuvastatin plasma concentration
These parameters provide crucial insights into the extent and rate of rosuvastatin absorption and bioavailability. By comparing these values across different administration scenarios, researchers could quantify the impact of antacids on rosuvastatin pharmacokinetics.
Significant Findings: The Impact of Simultaneous Antacid Administration
The study revealed a substantial interaction when rosuvastatin and antacids were administered simultaneously. This co-administration led to significant reductions in both key pharmacokinetic parameters:
- AUC(0-t) reduced by 54% (90% confidence interval [CI]: 0.40-0.53)
- C(max) reduced by 50% (90% CI: 0.41-0.60)
What do these reductions mean for patients? A decrease of this magnitude in AUC(0-t) and C(max) suggests that simultaneous antacid administration could significantly reduce the systemic exposure to rosuvastatin, potentially compromising its therapeutic efficacy.
Implications for Clinical Practice
These findings highlight the importance of considering the timing of antacid administration in patients taking rosuvastatin. Healthcare providers should be aware of this interaction and advise patients accordingly to ensure optimal therapeutic outcomes.
Mitigating the Interaction: The Effect of Separated Administration
Recognizing the potential for interaction, the study also investigated whether separating the administration of rosuvastatin and antacids could mitigate these effects. When antacids were given 2 hours after rosuvastatin, the impact on pharmacokinetics was notably reduced:
- AUC(0-t) reduced by 22% (90% CI: 0.68-0.90)
- C(max) reduced by 16% (90% CI: 0.70-1.01)
While still present, the interaction was substantially less pronounced compared to simultaneous administration. This finding suggests that separating the intake of rosuvastatin and antacids by at least 2 hours could be an effective strategy to minimize the interaction.
Clinical Recommendations
Based on these results, healthcare providers might consider advising patients to:
- Take rosuvastatin at least 2 hours before any antacid medications
- If antacids are needed, wait at least 2 hours after taking rosuvastatin
- Monitor lipid levels closely if antacids are used regularly
Limitations and Future Directions
While this study provides valuable insights into the rosuvastatin-antacid interaction, it’s important to note some limitations:
- The study did not assess the effect of repeated antacid administration
- Only healthy male volunteers were included, potentially limiting generalizability
- The long-term clinical implications of this interaction were not evaluated
These limitations open avenues for future research. Studies investigating the effects of chronic antacid use, diverse patient populations, and long-term clinical outcomes would further enhance our understanding of this interaction.
Potential Areas for Further Investigation
- Impact of different antacid formulations on rosuvastatin pharmacokinetics
- Effects in patients with various comorbidities or on multiple medications
- Long-term cardiovascular outcomes in patients co-administering rosuvastatin and antacids
- Exploration of potential mechanisms underlying the observed interaction
Broader Implications: Drug Interactions in Lipid Management
The findings of this study extend beyond the specific interaction between rosuvastatin and antacids. They underscore the importance of considering potential drug interactions in the management of dyslipidemia and cardiovascular risk.
Key Considerations for Healthcare Providers
- Comprehensive medication review for patients on lipid-lowering therapy
- Awareness of common over-the-counter medications that may interact with statins
- Patient education on proper timing and administration of medications
- Regular monitoring of lipid levels and adjustment of therapy as needed
How can healthcare providers optimize lipid management in the context of potential drug interactions? A multifaceted approach involving medication reconciliation, patient education, and vigilant monitoring is crucial for achieving optimal therapeutic outcomes.
Patient-Centered Approaches to Managing Rosuvastatin Therapy
Given the potential for interaction between rosuvastatin and antacids, adopting a patient-centered approach to medication management is essential. This involves not only educating patients about potential interactions but also working collaboratively to develop strategies that ensure optimal therapeutic benefit while minimizing risks.
Strategies for Enhancing Patient Adherence and Outcomes
- Provide clear, written instructions on medication timing and administration
- Discuss the importance of consistent medication schedules
- Encourage patients to maintain a medication diary
- Regularly review and update the patient’s complete medication list, including over-the-counter products
- Consider the use of medication reminder apps or devices
- Schedule follow-up appointments to assess therapy effectiveness and address any concerns
How can healthcare providers empower patients to take an active role in managing their rosuvastatin therapy? By fostering open communication, providing comprehensive education, and tailoring management strategies to individual patient needs and preferences, providers can enhance treatment adherence and outcomes.
Advancing Pharmacokinetic Research: Lessons from the Rosuvastatin-Antacid Study
The investigation into the interaction between rosuvastatin and antacids offers valuable insights for future pharmacokinetic research. This study exemplifies the importance of considering not only the presence of drug interactions but also the nuances of timing and administration in medication management.
Key Takeaways for Future Research
- Importance of assessing both simultaneous and separated administration scenarios
- Value of crossover study designs in minimizing inter-individual variability
- Need for comprehensive evaluation of pharmacokinetic parameters
- Relevance of studying common over-the-counter medications in drug interaction research
How can these insights shape future pharmacokinetic studies? Researchers may consider incorporating multiple administration scenarios, evaluating a broader range of pharmacokinetic parameters, and including diverse patient populations to enhance the clinical applicability of their findings.
Technological Advancements in Drug Interaction Management
As our understanding of drug interactions grows, so does the potential for leveraging technology to enhance medication management. The findings from studies like the rosuvastatin-antacid interaction can inform the development of sophisticated tools and systems to support both healthcare providers and patients.
Emerging Technologies in Medication Management
- AI-powered drug interaction checkers
- Smart medication dispensers with timing alerts
- Mobile apps for personalized medication scheduling
- Electronic health records with integrated interaction alerts
- Wearable devices for real-time medication reminders
How might these technologies transform the landscape of lipid management and drug interaction prevention? By providing real-time, personalized guidance and alerts, these tools have the potential to significantly reduce the risk of adverse drug interactions and enhance therapeutic outcomes.
Global Perspectives on Statin-Antacid Interactions
While this study focused specifically on rosuvastatin, it raises important questions about potential interactions between other statins and antacids. Given the global prevalence of both statin use and antacid consumption, understanding these interactions has far-reaching implications for public health.
Considerations for Global Health Policy
- Variation in prescribing practices and medication availability across countries
- Differences in dietary habits that may influence medication absorption
- Cultural factors affecting medication adherence and timing
- Economic considerations in medication choice and administration
How can global health organizations address the challenges posed by statin-antacid interactions? Developing international guidelines, promoting cross-cultural research, and fostering collaboration between healthcare systems could help create a more unified approach to managing these interactions worldwide.
The Role of Pharmacists in Managing Rosuvastatin-Antacid Interactions
Pharmacists play a crucial role in identifying and managing potential drug interactions, including those between rosuvastatin and antacids. Their expertise and direct contact with patients position them uniquely to provide guidance and ensure safe medication use.
Key Responsibilities of Pharmacists
- Screening for potential interactions during medication dispensing
- Providing patient education on proper medication timing and administration
- Collaborating with prescribers to optimize medication regimens
- Conducting medication therapy management sessions
- Monitoring for adverse effects and therapeutic outcomes
How can pharmacists enhance their role in managing rosuvastatin-antacid interactions? By staying informed about the latest research, utilizing drug interaction databases, and developing patient education materials, pharmacists can significantly contribute to safer and more effective lipid management strategies.
Integrating Research Findings into Clinical Practice Guidelines
The insights gained from studies like the rosuvastatin-antacid interaction trial have the potential to influence clinical practice guidelines. These guidelines play a crucial role in standardizing care and ensuring that healthcare providers have access to the most up-to-date, evidence-based recommendations.
Steps for Guideline Integration
- Critical appraisal of research findings by expert panels
- Assessment of the strength of evidence and clinical relevance
- Development of specific recommendations for medication timing and administration
- Integration of recommendations into existing lipid management guidelines
- Dissemination of updated guidelines to healthcare providers
- Implementation of guideline recommendations in clinical decision support systems
How can professional organizations ensure that new findings are quickly and effectively incorporated into clinical practice? By establishing streamlined processes for guideline updates, leveraging digital platforms for dissemination, and providing ongoing education to healthcare providers, organizations can facilitate the rapid translation of research into practice.
The Future of Personalized Lipid Management
As our understanding of drug interactions and individual patient factors grows, the field of lipid management is moving towards increasingly personalized approaches. The findings from studies like the rosuvastatin-antacid interaction trial contribute to this evolution by highlighting the importance of considering individual patient characteristics and medication regimens.
Emerging Trends in Personalized Lipid Management
- Pharmacogenomic testing to guide statin selection and dosing
- Integration of artificial intelligence for predicting drug interactions
- Development of novel drug delivery systems to minimize interactions
- Tailored lifestyle interventions to complement pharmacological therapy
- Precision monitoring of lipid levels and cardiovascular risk factors
How might these advancements shape the future of lipid management? By combining cutting-edge technology with a deep understanding of individual patient factors, healthcare providers may soon be able to offer truly personalized treatment strategies that maximize efficacy while minimizing the risk of adverse interactions.
The effect of a combination antacid preparation containing aluminium hydroxide and magnesium hydroxide on rosuvastatin pharmacokinetics
Clinical Trial
. 2008 Apr;24(4):1231-5.
doi: 10.1185/030079908×280662.
Epub 2008 Mar 19.
Paul D Martin
1
, Dennis W Schneck, Aaron L Dane, Michael J Warwick
Affiliations
Affiliation
- 1 AstraZeneca, Alderley Park, Cheshire, UK. [email protected]
PMID:
18355422
DOI:
10.1185/030079908×280662
Clinical Trial
Paul D Martin et al.
Curr Med Res Opin.
2008 Apr.
. 2008 Apr;24(4):1231-5.
doi: 10.1185/030079908×280662.
Epub 2008 Mar 19.
Authors
Paul D Martin
1
, Dennis W Schneck, Aaron L Dane, Michael J Warwick
Affiliation
- 1 AstraZeneca, Alderley Park, Cheshire, UK. [email protected]
PMID:
18355422
DOI:
10.1185/030079908×280662
Abstract
Objective:
Rosuvastatin, a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor used for the treatment of dyslipidaemia, may be co-administered with antacids in clinical practice. This trial assessed the effect of simultaneous and separated administration of an antacid preparation containing aluminium hydroxide 220 mg/5 mL and magnesium hydroxide 195 mg/5 mL (co-magaldrox 195/220) on the pharmacokinetics of rosuvastatin.
Research design and methods:
A randomised, open-label, three-way crossover trial was performed. Healthy male volunteers (n = 14) received a single dose of rosuvastatin 40 mg alone, rosuvastatin 40 mg plus 20 mL antacid suspension taken simultaneously, and rosuvastatin 40 mg plus 20 mL antacid suspension taken 2 h after rosuvastatin on three separate occasions with a washout of > or = 7 days between each.
Main outcome measures:
The primary parameters were area under the rosuvastatin plasma concentration-time curve from time zero to the last quantifiable concentration (AUC(0-t)) and maximum observed rosuvastatin plasma concentration (C(max)) in the absence and presence of antacid.
Results:
When rosuvastatin and antacid were given simultaneously, the antacid reduced the rosuvastatin AUC(0-t) by 54% (90% confidence interval [CI] for the treatment 0.40-0.53) and C(max) by 50% (90% CI 0.41-0.60). When the antacid was given 2 h after rosuvastatin, the antacid reduced the rosuvastatin AUC(0-t) by 22% (90% CI 0.68-0.90) and the C(max) by 16% (90% CI 0.70-1.01). The effect of repeated antacid administration was not studied and it cannot be discounted that this may have resulted in a stronger interaction than that observed here.
Conclusions:
Simultaneous dosing with rosuvastatin and antacid resulted in a decrease in rosuvastatin systemic exposure of approximately 50%. This effect was mitigated when antacid was administered 2 h after rosuvastatin.
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Crestor (Rosuvastatin) – Side Effects, Interactions, Uses, Dosage, Warnings
uses
What is Crestor (Rosuvastatin) used for?
- Hyperlipidemia
- Hyperlipoproteinemia Type III (Elevated beta-VLDL + IDL)
- Homozygous Familial Hypercholesterolemia
- Hypertriglyceridemia
- Atherosclerosis
- Prevention of Cardiovascular Disease
- Heterozygous Familial Hypercholesterolemia
warnings
What is the most important information I should know about Crestor (Rosuvastatin)?
You should not take rosuvastatin if you are allergic to it, or if you have:
- liver disease; or
- if you are pregnant or breast-feeding.
Do not take rosuvastatin if you are pregnant. It could harm the unborn baby. Use effective birth control to prevent pregnancy while you are taking rosuvastatin. Stop taking rosuvastatin and tell your doctor right away if you become pregnant.
Do not breastfeed while you are taking rosuvastatin.
Tell your doctor if you have ever had:
- liver problems;
- kidney disease;
- a thyroid disorder;
- a habit of drinking more than 2 alcoholic beverages per day;
- if you are of Asian descent; or
- if you are 65 or older.
Rosuvastatin can cause the breakdown of muscle tissue, which can lead to kidney failure. This happens more often in women, in older adults, or people who have kidney disease or poorly controlled hypothyroidism (underactive thyroid).
People of Asian descent may absorb rosuvastatin at a higher rate than other people. Make sure your doctor knows if you are Asian. You may need a lower than normal starting dose.
User Reviews & Rating
Overall rating for Crestor (Rosuvastatin)
2.6
out of 5
Side Effects
Easy to Use
Effectiveness
Read Crestor (Rosuvastatin) Reviews
Side Effects
What are the side effects of Crestor (Rosuvastatin)?
Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Call your doctor at once if you have:
- unexplained muscle pain, tenderness, or weakness;
- muscle weakness in your hips, shoulders, neck, and back;
- trouble lifting your arms, trouble climbing or standing;
- confusion, memory problems; or
- liver problems–upper stomach pain, tiredness, loss of appetite, dark urine, jaundice (yellowing of the skin or eyes).
Common side effects may include:
- headache;
- weakness;
- muscle aches; or
- nausea, stomach pain.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Pregnancy & Breastfeeding
Can I take Crestor (Rosuvastatin) if I’m pregnant or breastfeeding?
Contraindicated in pregnancy
Based on FDA pregnancy categories
Do not take rosuvastatin if you are pregnant. It could harm the unborn baby. Use effective birth control to prevent pregnancy while you are taking rosuvastatin. Stop taking rosuvastatin and tell your doctor right away if you become pregnant.
Do not breastfeed while you are taking rosuvastatin.
Interactions
What drugs and food should I avoid while taking Crestor (Rosuvastatin)?
Avoid eating foods high in fat or cholesterol, or rosuvastatin will not be as effective.
Avoid drinking alcohol. It can raise triglyceride levels and may increase your risk of liver damage.
Some antacids can make it harder for your body to absorb rosuvastatin. Avoid taking an antacid that contains aluminum or magnesium within 2 hours after taking rosuvastatin.
Dosage Guidelines & Tips
How to take Crestor (Rosuvastatin)?
Use Crestor (Rosuvastatin) exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.
What should I do if I missed a dose of Crestor (Rosuvastatin)?
Take the medicine as soon as you can, but skip the missed dose if you are more than 12 hours late for the dose. Do not use two doses at one time.
Overdose Signs
What happens if I overdose on Crestor (Rosuvastatin)?
If you think you or someone else may have overdosed on: Crestor (Rosuvastatin), call your doctor or the Poison Control center
(800) 222-1222
If someone collapses or isn’t breathing after taking Crestor (Rosuvastatin), call 911
911
What to Expect
Rosuvastatin starts to lower cholesterol levels within about a week, but it may take up to a month before it works completely.
You may have to stay on rosuvastatin for the rest of your life. You’ll only experience the benefits while you take this medicine. Your cholesterol levels may go back up if you stop using rosuvastatin.
Secondary Uses
Statins, including rosuvastatin, have been studied or used to treat other medical conditions that they aren’t FDA-approved for. For example, rosuvastatin is sometimes given to patients after a heart or kidney transplant to improve outcomes.
Images
CRESTOR 10
Color: pink
Shape: round
Form: film coated
Imprint: CRESTOR 10
CRESTOR 20
Color: pink
Shape: round
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CRESTOR, 40
Color: pink
Shape: oval
Form: film coated
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Rosuvastatin: instruction, price, analogues | Biofarm
film-coated tablets (Rosuvastatin)
Manufacturer:
Biofarm
Composition and form of release
You can pay for medicines with a card pidtrimka
Classification
Atherosclerosis of the aorta | ICD I70. 0 |
Atherosclerosis of the arteries of the extremities | ICD I70.2 |
Atherosclerotic heart disease | ICD I25.1 |
Hypertensive heart disease without (congestive) heart failure | ICD I11.9 |
Hypertension (AH) with heart disease and heart failure (HF) | ICD I11.0 |
Other specified lesions of cerebral vessels | ICD I67.8 |
Other forms of angina pectoris | ICD I20.8 |
Cerebral infarction caused by thrombosis of the cerebral arteries | ICD I63.3 |
Post-infarction coronary heart disease (CHD), (past myocardial infarction) | ICD I25.2 |
Ischemic heart disease with hypertension (CHD with HT) | ICD I25. 9 |
Ischemic heart disease with angina pectoris | ICD I25.0 |
Unstable angina Manual of cardiology (ed. V.N. Kovalenko, 2008) … Clinical protocol for the provision of medical care to patients with acute coronary syndrome without ST segment elevation (MI without Q wave and unstable angina pectoris) | ICD I20.0 |
Acute transmural (with Q wave) infarction of the inferior myocardial wall Manual of cardiology (ed. V.N. Kovalenko, 2008) … Clinical protocol for the provision of medical care to patients with acute coronary syndrome with ST segment elevation (MI with Q wave) | ICD I21. 1 |
Acute transmural infarction of the anterior myocardial wall Manual of cardiology (ed. V.N. Kovalenko, 2008) … Clinical protocol for the provision of medical care to patients with acute coronary syndrome without ST segment elevation (MI without Q wave and unstable angina pectoris) | ICD I21.0 |
Persistent atrial fibrillation Manual of cardiology (edited by V.N. Kovalenko, 2008) … Clinical protocol for providing medical care to patients with atrial fibrillation (flutter) | ICD I48.1 |
Recurrent myocardial infarction, unspecified Manual of cardiology (ed. V.N. Kovalenko, 2008) … Clinical protocol for the provision of medical care to patients with acute coronary syndrome without ST segment elevation (MI without Q wave and unstable angina pectoris) | ICD I22.9 |
Consequences of cerebral infarction | ICD I69.3 |
Angina | ICD I20.9 |
Juvenile arterial hypertension | ICD I10 |
Date added: 07/05/2023
© Compendium 2019
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5 herbs and spices that can reduce the effect of drugs
- Health
Many seemingly harmless herbs and herbal preparations can interact with various drugs and reduce their effect. So, when prescribing dietary supplements for yourself, you should be very careful.
March 4, 20231
- Source:
- iStockphoto
We know about the health benefits of garlic and green tea, both recognized as powerful antioxidants. It is very useful to use them in the diet in moderation, but it can be unsafe to get involved in preparations based on them. And not only them. There are other herbs and spices that seriously affect the effectiveness of the pharmaceutical preparations you take, writes ProNews.
Turmeric
This spice and dietary supplements with curcumin are often called “fool’s gold”. Science considers its antitumor, anti-inflammatory and antibacterial properties to be only potential. But the interaction of curcumin with drugs can even be dangerous.
There is evidence that curcumin may reduce the effect of many antidepressants and neuroleptics. It is also known to interact with anticoagulants, antacids, drugs to control blood pressure.
– Whole turmeric, turmeric extract or pure curcumin are credited with at least 175 different beneficial physiological effects and more than 600 different indications, explains renowned physician, toxicologist Alexei Vodovozov. “But if you search the available databases for relevant studies, it turns out that of them are at the preclinical stage, , that is, cell cultures and laboratory animals (mice and rats). And the results found are of interest mainly to mice and rats, because they are transferred to humans very, very rarely.
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Garlic
Garlic extract can reduce the concentration of cardiac glycosides, glucocorticoids – drugs that transport P-glycoprotein protein across the cell membrane – such as colchicine, quinidine, desloratadine, digoxin, rosuvastatin and others , writes ProNews
Garlic extract can also thin the blood like aspirin, which can be a problem if you are taking blood thinners.
– It happens that people take both aspirin and anticoagulants, then the risk of bleeding increases exponentially. I have had such cases. People go to the hospital to the surgeons on the operating table, because they have gastrointestinal bleeding, , doctor Boris Shelyapin told Doctor Peter earlier.
Green tea
Everyone knows about the benefits of green tea – it has antioxidant properties, anti-inflammatory, promotes the expansion of cerebral vessels, improves its nutrition, oxygen supply. All this is true, if you drink 2-3 cups of quality green tea a day. Although it is not shown to everyone – after all, a drink can lower blood pressure and harm ulcers.
Taking green tea extract as a dietary supplement can also be hazardous to health. There is evidence that green tea extract may reduce the effectiveness of some statins and some beta-blockers used to treat hypertension. Also concentrated green tea supplements may interact with some vasoconstrictors.
Thistle or milk thistle
This plant is believed to have many beneficial properties, and the active substance silymarin contained in it is called the first “protector” of the liver.